RS52851B - Cyclopropyl amide derivatives targeting the histamine h3 receptor - Google Patents

Cyclopropyl amide derivatives targeting the histamine h3 receptor

Info

Publication number
RS52851B
RS52851B RS20130280A RSP20130280A RS52851B RS 52851 B RS52851 B RS 52851B RS 20130280 A RS20130280 A RS 20130280A RS P20130280 A RSP20130280 A RS P20130280A RS 52851 B RS52851 B RS 52851B
Authority
RS
Serbia
Prior art keywords
c3alkyl
c6alkyl
alkyl
formula
heteroatom selected
Prior art date
Application number
RS20130280A
Other languages
Serbian (sr)
Inventor
Andrew Griffin
Original Assignee
Astrazeneca Ab.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42631518&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS52851(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab. filed Critical Astrazeneca Ab.
Publication of RS52851B publication Critical patent/RS52851B/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/104—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/108—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Jedinjenje formule I, ili njegovi enantiomeri ili dijastereomeri, ili farmaceutski prihvatljive soli formule I ili njihovi enantiomeri ili dijastereomeri, ili njihove smeše:naznačeno time da:R1 je aril, heteroaril, -C1-C6alkil-C1-C3alkoksi, -C1-C6alkil-hidroksi, -C1-C6alkil-C(=O)-NR11R12, -S(=O)2NR11R12, heterocikal, cijano, haloalkil, -C(=O)NR11R12, alkoksi, ili halogen;R2 je C1-C6alkil ili C3-C6cikloalkil;R3, R4, R5, R6, R7, R8, R9, i R10 su svaki nezavisno izabrani od H i C1-C3alkila; iR11 i R12 su svaki nezavisno izabrani od H, -C1-C6alkila, -C1-C3alkil-C1-C3alkoksi, 5-članog heterocikloalkila koji sadrži barem jedan heteroatom izabran od O i N, 6-članog heterocikloalkila koji sadrži barem jedan heteroatom izabran od O i N, -(C1-C3alkil)-(5-člani heteroaril koji sadrži barem jedan heteroatom izabran od O i N), -(C1-C3alkil)-(6-člani heteroaril koji sadrži barem jedan heteroatom izabran od O i N),haloalkil, ili R11, R12 i azot na koji su vezani udružuju se i grade heterocikloalkil izabran od pirolidinila, morfolinila, piperidinila, i piperazinila, gde je pomenuti heterocikloalkil po izboru supstituisan sa najmanje jednim supstituentom izabranim iz -C1-C3alkila i -C1-C6alkil-C1-C3alkoksi; i pod pretpostavkom da:i) barem jedan od R3, R4, R5, R6, R7, R8, R9, i R10 je C1-C3alkil;ii) formula I nijekada R1 je -C(=O)NR11R12 grupa meta-vezana na fenil, R2 je izopropil, te R11 i R12 su H; iiii) formula I nije u cis konfiguraciji na ciklopropanu.Prijava sadrži još 14 patentnih zahteva.Compound of formula I, or enantiomers or diastereomers thereof, or pharmaceutically acceptable salts of formula I, or enantiomers or diastereomers thereof, or mixtures thereof: wherein: R 1 is aryl, heteroaryl, -C 1 -C 6 alkyl-C 1 -C 3 alkoxy, -C 1 -C 6 alkyl- hydroxy, -C1-C6alkyl-C (= O) -NR11R12, -S (= O) 2NR11R12, heterocycle, cyano, haloalkyl, -C (= O) NR11R12, alkoxy, or halogen, R2 is C1-C6alkyl or C3- R3, R4, R5, R6, R7, R8, R9, and R10 are each independently selected from H and C1-C3alkyl; iR11 and R12 are each independently selected from H, -C1-C6alkyl, -C1-C3alkyl-C1-C3alkoxy, 5-membered heterocycloalkyl containing at least one heteroatom selected from O and N, 6-membered heterocycloalkyl containing at least one heteroatom selected from O and N, - (C1-C3alkyl) - (5-membered heteroaryl containing at least one heteroatom selected from O and N), - (C1-C3alkyl) - (6-membered heteroaryl containing at least one heteroatom selected from O and N) ), haloalkyl, or R 11, R 12 and the nitrogen to which they are attached combine to form a heterocycloalkyl selected from pyrrolidinyl, morpholinyl, piperidinyl, and piperazinyl, wherein said heterocycloalkyl is optionally substituted with at least one substituent selected from -C 1 -C 3 alkyl and -C 1 -C6alkyl-C1-C3alkoxy; and provided that: i) at least one of R 3, R 4, R 5, R 6, R 7, R 8, R 9, and R 10 is C 1 -C 3 alkyl, ii) formula I never R 1 is a -C (= O) NR 11 R 12 group meta-attached to phenyl, R2 is isopropyl, and R11 and R12 are H; iiii) formula I is not in the cis configuration on cyclopropane. The application contains 14 more claims.

RS20130280A 2009-02-20 2010-02-19 Cyclopropyl amide derivatives targeting the histamine h3 receptor RS52851B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15406709P 2009-02-20 2009-02-20
PCT/SE2010/050191 WO2010096011A1 (en) 2009-02-20 2010-02-19 Cyclopropyl amide derivatives targeting the histamine h3 receptor

Publications (1)

Publication Number Publication Date
RS52851B true RS52851B (en) 2013-12-31

Family

ID=42631518

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20130280A RS52851B (en) 2009-02-20 2010-02-19 Cyclopropyl amide derivatives targeting the histamine h3 receptor

Country Status (39)

Country Link
US (3) US8993577B2 (en)
EP (1) EP2398780B1 (en)
JP (2) JP5666480B2 (en)
KR (1) KR20110126628A (en)
CN (2) CN104398516A (en)
AR (1) AR075531A1 (en)
AU (1) AU2010216454B2 (en)
BR (1) BRPI1007817A2 (en)
CA (1) CA2752796A1 (en)
CO (1) CO6400219A2 (en)
CR (1) CR20110447A (en)
CU (2) CU20110161A7 (en)
DK (1) DK2398780T3 (en)
DO (1) DOP2011000270A (en)
EA (2) EA020093B1 (en)
EC (1) ECSP11011280A (en)
ES (1) ES2416464T3 (en)
HK (2) HK1164863A1 (en)
HN (1) HN2011002261A (en)
HR (1) HRP20130579T1 (en)
IL (1) IL214277A (en)
ME (1) ME01619B (en)
MX (1) MX2011008280A (en)
NI (1) NI201100160A (en)
NZ (1) NZ595248A (en)
PE (2) PE20151281A1 (en)
PL (1) PL2398780T3 (en)
PT (1) PT2398780E (en)
RS (1) RS52851B (en)
SA (1) SA110310136B1 (en)
SG (1) SG173449A1 (en)
SI (1) SI2398780T1 (en)
SM (1) SMT201300077B (en)
SV (1) SV2011004008A (en)
TW (1) TW201039825A (en)
UA (1) UA108841C2 (en)
UY (1) UY32460A (en)
WO (1) WO2010096011A1 (en)
ZA (1) ZA201106821B (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090024811A (en) * 2006-06-23 2009-03-09 아보트 러보러터리즈 Cyclopropyl amine derivatives as histamin h3 receptor modulators
US9108948B2 (en) * 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
TWI432422B (en) * 2007-08-22 2014-04-01 Astrazeneca Ab Cyclopropyl amide derivatives
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
CA2789884A1 (en) * 2010-02-18 2011-08-25 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative
SG183274A1 (en) * 2010-02-18 2012-09-27 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
WO2012037258A1 (en) 2010-09-16 2012-03-22 Abbott Laboratories Processes for preparing 1,2-substituted cyclopropyl derivatives
SG11201808220VA (en) 2016-03-22 2018-10-30 Merck Sharp & Dohme Allosteric modulators of nicotinic acetylcholine receptors
EP4215534A1 (en) 2020-09-18 2023-07-26 Sumitomo Pharma Co., Ltd. Amine derivative

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL297170A (en) * 1963-04-04 1900-01-01
NL128365C (en) 1963-11-05
US3449427A (en) * 1965-06-03 1969-06-10 Smithkline Corp Aminocyclopropane derivatives of 5h-dibenzo(a,d)cycloheptenes
US3697506A (en) 1970-08-07 1972-10-10 Pfizer Crystalline alkali metal salts of {60 -carboxybenzylpenicillin and process therefor
US3686335A (en) * 1970-12-21 1972-08-22 Smith Kline French Lab 5-vinyl-5h-di benzo(a,d)cycloheptenes
US4432987A (en) 1982-04-23 1984-02-21 Pfizer Inc. Crystalline benzenesulfonate salts of sultamicillin
US4547505A (en) * 1983-03-25 1985-10-15 Degussa Aktiengesellschaft N-Phenyl-N-'-cycloalkylalkanoylpiperazine useful as analgetics and process for its production
CS244821B2 (en) 1983-06-16 1986-08-14 Boehringer Ingelheim Ltd Production method of new substituted phenylalkyl(piperazinyl or homopiperazinyle)-prpylureas or thioureas
DE3418167A1 (en) 1984-05-16 1985-11-21 Bayer Ag, 5090 Leverkusen Use of amides for improving the crop plant compatibility of herbicidally active heteroaryloxyacetamides
DE3600288A1 (en) 1986-01-08 1987-07-16 Bayer Ag USE OF AMIDES FOR IMPROVING THE CROP PLANT TOLERABILITY OF HERBICIDE-ACTIVE SULFONYL URINE DERIVATIVES
DE3618004A1 (en) 1986-05-28 1987-12-03 Bayer Ag Use of amides for improving the crop plant tolerance of herbicidally active sulphonyliso(thio)urea derivatives
CA2071897A1 (en) 1989-12-28 1991-06-29 Richard A. Glennon Sigma receptor ligands and the use thereof
DE69013131T2 (en) * 1989-12-29 1995-05-24 Banyu Pharma Co Ltd 2- (2-Cyclopropylpyrrolidin-4-ylthio) carbapenem derivatives.
AU2505392A (en) 1991-08-22 1993-03-16 Monsanto Company Safening herbicidal pyrazolylsulfonylureas
DE4131139A1 (en) 1991-09-19 1993-03-25 Bayer Ag METHOD FOR PRODUCING 1-FLUOR-CYCLOPROPAN-1-CARBONIC ACID
AU694419B2 (en) 1993-03-12 1998-07-23 Zoetis P&U Llc Crystalline ceftiofur free acid
BR9509760A (en) 1994-11-23 1998-06-30 Neurogen Corp Compound
US5604253A (en) 1995-05-22 1997-02-18 Merck Frosst Canada, Inc. N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
US5859246A (en) 1997-01-30 1999-01-12 Neurogen Corporation 1-phenyl-4-benzylpiperazines: dopamine receptor subtype specific ligands
AU6179998A (en) 1997-02-24 1998-09-09 Zymogenetics Inc. Calcitonin mimetics
US6160134A (en) 1997-12-24 2000-12-12 Bristol-Myers Squibb Co. Process for preparing chiral cyclopropane carboxylic acids and acyl guanidines
UA59433C2 (en) 1998-01-27 2003-09-15 Авентіс Фармасьютікалс Продактс Інк. Substituted oxoazaheterocyclyl inhibitors of xa factor
US6268367B1 (en) 1998-02-23 2001-07-31 Zymogenetics, Inc. Piperazine derivatives for treating bone deficit conditions
WO2000000492A1 (en) 1998-06-26 2000-01-06 Chugai Seiyaku Kabushiki Kaisha FINE POWDER OF L-α-AMINOADIPIC ACID DERIVATIVE, ORAL SOLID PREPARATIONS CONTAINING THE SAME, AND METHOD FOR TREATMENT OF BULK POWDERS
US6284761B1 (en) * 1999-01-08 2001-09-04 Neurogen Corporation 1-phenyl-4-(1-[2-aryl]cyclopropyl)methylpiperazines: dopamine receptor ligands
WO2000040572A1 (en) 1999-01-08 2000-07-13 Neurogen Corporation 1-phenyl-4-(1-[2-aryl]cyclopropyl) methylpiperazines: dopamine receptor ligands
WO2000076993A1 (en) 1999-06-16 2000-12-21 Takeda Chemical Industries, Ltd. Benzazepine derivatives, process for the preparation of the same and uses thereof
WO2001022963A1 (en) 1999-09-27 2001-04-05 Merck & Co., Inc. Method of preventing osteoporosis
US20020048610A1 (en) 2000-01-07 2002-04-25 Cima Michael J. High-throughput formation, identification, and analysis of diverse solid-forms
EP1294685A1 (en) 2000-06-29 2003-03-26 Abbott Laboratories Aryl phenycyclopropyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
US6521619B2 (en) * 2000-06-29 2003-02-18 Icos Corporation Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents
WO2002008221A2 (en) 2000-07-20 2002-01-31 Neurogen Corporation Capsaicin receptor ligands
EP1346972A4 (en) 2000-12-25 2005-06-01 Ajinomoto Kk Process for producing optically active halohydrin compound
DK1379520T3 (en) * 2001-02-23 2006-08-21 Merck & Co Inc N-substituted non-aryl heterocyclic NMDA / NR2B antagonists
JP2005502623A (en) 2001-07-02 2005-01-27 ノボ　ノルディスク　アクティーゼルスカブ Substituted piperazines and diazepanes
WO2003014110A1 (en) 2001-08-08 2003-02-20 Takeda Chemical Industries, Ltd. Benzazepine derivative, process for producing the same, and use
AU2002331885B2 (en) 2001-09-26 2007-07-26 Merck & Co., Inc. Crystalline forms of ertapenem sodium
AU2002363236A1 (en) 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
US6861432B2 (en) * 2001-11-23 2005-03-01 Schering Aktiengesellschaft Piperazine derivatives that destabilize androgen receptors
RU2004131204A (en) 2002-03-22 2005-04-10 Эл Джи Лайф Сайенсиз Лтд. (Kr) NEW CRYSTALLINE FORMS (2S) -N-5- [AMINO (IMINO) METHYL] -2-THIENYLMETHYL-1- (2R) - [(CARBOXYMETHYL) AMINO] -3, 3-D IFENYLPROPANOYL-2-PYRANOID
AU2003236686A1 (en) 2002-06-07 2003-12-22 Altana Pharma Ag 4,5-dihydro-imidazo(4,5,1-j) quinolin-6-ones as parp inhibitors
US20040077618A1 (en) * 2002-10-22 2004-04-22 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
US20040209858A1 (en) * 2002-10-22 2004-10-21 Bennani Youssef L. Cycloalkylamides and their therapeutic applications
WO2004046110A1 (en) 2002-11-15 2004-06-03 Yamanouchi Pharmaceutical Co., Ltd. Antagonist to melanin-concentrating hormone receptor
AU2003296993A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Cyclopropyl compounds as ccr5 antagonists
ES2311152T3 (en) 2003-04-23 2009-02-01 Glaxo Group Limited DERIVATIVES OF PIPERAZINE AND ITS USE FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISEASES.
EP2385041B1 (en) 2003-05-01 2013-09-18 Bristol-Myers Squibb Company Pyrazole-amine compounds useful as kinase inhibitors
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
CA2549660A1 (en) * 2003-12-15 2005-06-30 Japan Tobacco Inc. Cyclopropane compounds and pharmaceutical use thereof
ATE537830T1 (en) 2004-07-06 2012-01-15 Xenon Pharmaceuticals Inc NICOTINAMIDE DERIVATIVES AND THEIR USE AS THERAPEUTICS
TW200621760A (en) 2004-09-09 2006-07-01 Mitsubishi Pharma Corp 2-morpholino-4-pyrimidone compound
EP1805164B9 (en) 2004-09-29 2011-09-07 Mitsubishi Tanabe Pharma Corporation 6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors
ATE387202T1 (en) 2004-10-15 2008-03-15 Glaxo Group Ltd PYRROLIDINE DERIVATIVES AS HISTAMINE RECEPTOR LIGANDS
AU2005322173A1 (en) 2004-12-27 2006-07-06 Astrazeneca Ab Pyrazolone compounds as metabotropic glutamate receptor agonists for the treatment of neurological and psychiatric disorders
EP1844052A1 (en) 2005-01-26 2007-10-17 Pharmacia & Upjohn Company LLC Thieno[2,3-d]pyrimidine compounds as inhibitors of adp-mediated platelets aggregation
JP2008530162A (en) 2005-02-15 2008-08-07 グラクソ グループ リミテッド Compounds that potentiate glutamate receptors and their use in medicine
KR101063585B1 (en) 2005-02-17 2011-09-07 아스텔라스세이야쿠 가부시키가이샤 Pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative
JP2008534488A (en) 2005-03-25 2008-08-28 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 4-piperazinylthieno [2,3-d] pyrimidine compounds as platelet aggregation inhibitors
CA2603041A1 (en) 2005-03-28 2006-10-05 Pharmacia & Upjohn Company Llc 4-piperazinylthieno [2, 3-d] pyrimidine compounds as platelet aggregation inhibitors
CA2602227A1 (en) 2005-03-28 2006-10-05 Michael Dalton Ennis 4-piperazinylthieno [2,3-d] pyrimidine compounds as platelet aggregation inhibitors
JP2008534573A (en) 2005-03-28 2008-08-28 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 4-piperazinothieno [2,3-D] pyrimidine compounds as platelet aggregation inhibitors
MX2008000745A (en) 2005-07-15 2008-03-14 Schering Corp Quinazoline derivatives useful in cancer treatment.
TW200740779A (en) 2005-07-22 2007-11-01 Mitsubishi Pharma Corp Intermediate compound for synthesizing pharmaceutical agent and production method thereof
WO2007016496A2 (en) 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
CA2622760C (en) * 2005-09-16 2012-12-04 Janssen Pharmaceutica N.V. Cyclopropyl amines as modulators of the histamine h3 receptor
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
RS52569B (en) 2005-10-31 2013-04-30 Janssen Pharmaceutica N.V. Processes for the preparation of cyclopropyl-amide derivatives
KR20080081178A (en) 2005-12-21 2008-09-08 버텍스 파마슈티칼스 인코포레이티드 Heterocyclic derivatives as modulators of ion channels
WO2007076140A2 (en) 2005-12-23 2007-07-05 University Of Cincinnati Treatment methods employing histamine h3 receptor antagonists, including betahistine
EP1976840A1 (en) * 2006-01-13 2008-10-08 F.Hoffmann-La Roche Ag Cyclohexyl piperazinyl methanone derivatives and their use as histamine h3 receptor modulators
CN101384581B (en) 2006-02-17 2013-09-18 弗·哈夫曼-拉罗切有限公司 Benzoyl-piperidine derivatives as 5HT2/D3 modulators
AU2007219709B2 (en) 2006-03-01 2012-08-16 Cementech Pty Ltd Matrix for masonry elements and method of manufacture thereof
JP2009132621A (en) 2006-03-13 2009-06-18 Ajinomoto Co Inc Method for producing cyclopropylamide compound
AU2007231594A1 (en) 2006-03-23 2007-10-04 Amgen Inc. 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases
JP5301270B2 (en) 2006-05-26 2013-09-25 株式会社カネカ Process for producing optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative and salt thereof
KR20090024811A (en) * 2006-06-23 2009-03-09 아보트 러보러터리즈 Cyclopropyl amine derivatives as histamin h3 receptor modulators
US9108948B2 (en) * 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
CA2657702A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs Wetenschappelijk Onderzoek E N Patieentenzorg Quinazolines and related heterocyclic comp0unds, and their therapeutic use
WO2008024284A2 (en) 2006-08-21 2008-02-28 Merck & Co., Inc. Sulfonylated piperazines as cannabinoid-1 receptor modulators
TW200828371A (en) 2006-09-21 2008-07-01 Matsushita Electric Ind Co Ltd Chip-type filter
DE102006056526A1 (en) 2006-11-30 2008-06-05 Archimica Gmbh Process for the stereoselective synthesis of chiral epoxides by ADH reduction of alpha-leaving group-substituted ketones and cyclization
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
WO2008147864A2 (en) * 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
EP2150115B1 (en) 2007-05-23 2013-09-18 Merck Sharp & Dohme Corp. Cyclopropyl pyrrolidine orexin receptor antagonists
ES2350511T3 (en) * 2007-06-11 2011-01-24 F. Hoffmann-La Roche Ag CYCLHEXILO DERIVATIVES
TWI432422B (en) * 2007-08-22 2014-04-01 Astrazeneca Ab Cyclopropyl amide derivatives
JP5362729B2 (en) 2007-10-04 2013-12-11 エフ．ホフマン−ラ ロシュ アーゲー Cyclopropylarylamide derivatives and uses thereof
PE20091313A1 (en) 2008-01-15 2009-09-03 Lilly Co Eli (R) -2- (4-CYCLOPROPANSULFONIL-PHENYL) -N-PIRAZIN-2-IL-3- (TETRAHYDROPYRAN-4-IL) -PROPIONAMIDE CRYSTALLINE
DE102008049371A1 (en) 2008-03-06 2009-09-10 Mühlbauer Ag Device with an RFID transponder in an electrically conductive object and manufacturing method thereof
CA2721303C (en) 2008-05-08 2016-06-28 Evotec Ag Azetidines and cyclobutanes as histamine h3 receptor antagonists
JP2012503595A (en) 2008-07-28 2012-02-09 シダンスク ユニバーシティ Compounds for the treatment of metabolic diseases
CN101462980B (en) 2009-01-05 2013-01-09 扬州天辰精细化工有限公司 Industrial production method of 2,6-difluorobenzamide
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
CA2789884A1 (en) 2010-02-18 2011-08-25 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative
SG183274A1 (en) 2010-02-18 2012-09-27 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith

Also Published As

Publication number Publication date
WO2010096011A1 (en) 2010-08-26
DK2398780T3 (en) 2013-07-01
UY32460A (en) 2010-09-30
NZ595248A (en) 2014-01-31
MX2011008280A (en) 2011-08-24
SG173449A1 (en) 2011-09-29
US20150164889A1 (en) 2015-06-18
AU2010216454B2 (en) 2013-05-02
AU2010216454A1 (en) 2011-08-25
PL2398780T3 (en) 2013-08-30
ES2416464T3 (en) 2013-08-01
SI2398780T1 (en) 2013-08-30
CN102405213A (en) 2012-04-04
US20100216812A1 (en) 2010-08-26
NI201100160A (en) 2012-03-15
CA2752796A1 (en) 2010-08-26
IL214277A0 (en) 2011-09-27
SV2011004008A (en) 2012-01-06
EP2398780A1 (en) 2011-12-28
PE20151281A1 (en) 2015-10-04
EP2398780B1 (en) 2013-04-17
CO6400219A2 (en) 2012-03-15
SA110310136B1 (en) 2014-01-14
CN102405213B (en) 2014-11-19
HK1164863A1 (en) 2012-09-28
CN104398516A (en) 2015-03-11
ECSP11011280A (en) 2011-09-30
DOP2011000270A (en) 2012-08-31
CU20140013A7 (en) 2014-04-24
UA108841C2 (en) 2015-06-25
EP2398780A4 (en) 2012-09-19
US8993577B2 (en) 2015-03-31
BRPI1007817A2 (en) 2017-05-30
HRP20130579T1 (en) 2013-07-31
US20150164888A1 (en) 2015-06-18
TW201039825A (en) 2010-11-16
HK1208348A1 (en) 2016-03-04
JP2015071634A (en) 2015-04-16
HN2011002261A (en) 2014-07-31
JP5666480B2 (en) 2015-02-12
SMT201300077B (en) 2013-09-06
PT2398780E (en) 2013-06-25
PE20120063A1 (en) 2012-03-04
ME01619B (en) 2014-09-20
CR20110447A (en) 2011-09-19
EA020093B1 (en) 2014-08-29
KR20110126628A (en) 2011-11-23
JP2012518634A (en) 2012-08-16
AR075531A1 (en) 2011-04-06
EA201190140A1 (en) 2012-03-30
EA201490268A1 (en) 2015-07-30
ZA201106821B (en) 2012-06-26
IL214277A (en) 2015-08-31
CU20110161A7 (en) 2012-02-15

Similar Documents

Publication Publication Date Title
RS52851B (en) Cyclopropyl amide derivatives targeting the histamine h3 receptor
AR085615A1 (en) USEFUL FLUOROPIRIDINONE DERIVATIVES AS ANTIBACTERIAL AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
PE20170247A1 (en) PYRROLIDINE-2,5-DIONA DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS TO USE AS IDO1 INHIBITORS
AR094452A1 (en) HETEROCYCLIC COMPOUNDS REPLACED WITH AMIDA USEFUL AS MODULATORS OF THE ANSWERS OF IL-12, IL-23 AND / OR INFa
RS52261B (en) Amidophenoxyindazoles useful as inhibitors of c-met
AR066169A1 (en) DERIVATIVES OF BENZO-IMIDAZOLES, USEFUL FOR DISORDERS ASSOCIATED WITH THE ACTIVITY OF DGAT
PE20181304A1 (en) INDEOL N-SUBSTITUTE DERIVATIVES AS MODULATORS OF PGE2 RECEPTORS
EA201591429A1 (en) 2,3-DESIGNED DERIVATIVES OF 1-ACYL-4-AMINO-1,2,3,4-TETRAHYDROCHINOLINES AND THEIR APPLICATION AS A BROMODOMENE INHIBITORS
RS54506B1 (en) Picolinamide derivatives as kinase inhibitors
RS51674B (en) Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists
RS52562B (en) (3-aryl-piperazin-1-yl) derivatives of 6,7-dialkoxyquinazoline, 6,7-dialkoxyphtalazine and 6,7-dialkoxyisoquinoline
MY169179A (en) Novel piperidine compound or salt thereof
SMT201300085B (en) Pyrrole compounds
EA201591703A1 (en) SUBSTITUTED 2-ABABILITIES AND THEIR APPLICATION AS OREXIN RECEPTOR MODULATORS
EA201690019A1 (en) AMINOTRIASIN DERIVATIVE AND CONTAINING ITS PHARMACEUTICAL COMPOSITION
PE20080409A1 (en) COMPOUNDS THAT MODULATE IN THE CB2 RECEIVER
EA201591675A1 (en) SUBSTITUTED 7-ABABILITIES AND THEIR APPLICATION AS OREXIN RECEPTOR MODULATORS
NO20092770L (en) Novel aminopyrimidine derivatives as PLK1 inhibitors
RU2016135922A (en) THERAPEUTIC COMPOUNDS AND COMPOSITIONS
AR091271A1 (en) PIRROLOPIRIMIDONA AND PIRROLOPIRIDONA, TANQUIRASA INHIBITORS
JO3509B1 (en) P2x7 modulators
RS53246B (en) Imidazole derivatives as casein kinase inhibitors
EA200970793A1 (en) MODULATORS OF RECEPTORS ACTIVATED BY PROLIFERATORS PEROXIS
HRP20200395T1 (en) Isoxazole derivative as mutated isocitrate dehydrogenase 1 inhibitor
AR109991A1 (en) COMBINATION TREATMENTS THAT INCLUDE THE ADMINISTRATION OF IMIDAZOPIRAZINONES